Intravenous ultrashort-acting anesthetic composition



United States Patent 2,839,447 Patented June 17, 1958 fit INTRAVENGUS ULTRASHORT-AC'I'ENG ANESTHETFC CGMPOSITION Heinrich Gruber, Berlin, Germany, assignor to Rietielde Haen Aktiengesellschaft, Seelze, near Hannover, Germany, a German firm N Drawing. Application January 7, 1955 Serial No. 480,587

Claims. (Cl. 167-52) My invention relates to a liquid anesthetic agent for intravenous injection and, more particularly, to an agent of this type including a derivative of barbituric acid.

Anesthetics of this kind are employed for operations requiring a comparatively short period of time. It has been found, however, that the anesthetic agents contain ing derivatives of barbituric acid which have been used heretofore have certain disadvantages. Under certain circumstances they may cause motorous agitation, singultus, cyanosis and finally asphyia. Frequently, the patient will sleep afterwards for a considerable period of time and often after awaking will not be able physically to return to his home without aid, since he will have a dizzy feeling.

It is the object of the present invention to so improve the anesthetic agent containing a derivative of barbituric acid that the human body will be able to overcome the stupor induced by the drug in a shorter time than heretofore. I have found that this object may be attained by the admixture with the derivative of barbituric acid of a suitable quantity of glycerol. In lieu of the glycerol, 1,2 propanediol or 1,3 butanediol may be used Moreover, I add a certain amount of diethyl-ether which has the effect of stimulating breathing and metabolism whereby the decomposition of the drug in the human body will be expedited. Moreover, I add a certain amount of 1- phenyl-2.3-dimethyl-pyrazolone, a composition known as an analgetic under the name of Antipyrine.

The following proportions have been found to give the best results: From 4 to 7% of the sodium salt of the barbituric acid derivative, from 4 to 6% of the Antipyrine, from 4 to 6% and preferably substantially 5% glycerol, and from 2 to 5% diethyl-ether, the stated percentages referring to the weight with respect to that of the aqueous solution. The derivative of barbituric acid which gives the best results is the sodium salt of 5-beta-bromally- 5-isopropy1-N-methyl-barbituric acid which is used in a well known anesthetic agent for intravenous injection known by its trade name Eunarcon.

It is the effect of my novel drug that when the patient awakes from the anesthesia he will feel fit. Thirty minutes after the injection was made he is fully able to return to his home. Moreover, the anesthetic agent becomes eifective immediately upon the instant of injection so that the operation may be commenced directly thereafter. Thus, it will appear that my improved anesthetic agent is ultra short acting.

While the invention has been described in connection with several different embodiments thereof, it will be understood that it is capable of further modification, and this application is intended to cover any variations, uses, or adaptations of the invention following, in general, the principles of the invention and including such departures from the present disclosure as come within known or customary practice in the art to which the invention pertains, and as fall within the scope of the invention or the limits of the appended claims.

What I claim is:

1. A liquid anesthetic agent for intravenous injection comprising an aqueous solution of from. 4 to 7% by weight of the sodium salt of the 5-beta-bromallyi-5-isopropyl-N-rnethyl-barbituric acid, from 4 to 6% by weight of 1-phenyl-2.3-dimethyl-pyrazolone, from 2 to 5% by weight of diethyl-ether, and 5% by weight of a liquid selected from the group consisting of glycerol and of 1,2 propanediol and of 1,3 butanediol.

2. A liquid anesthetic agent for intravenous injection comprising an aqueous solution of from 4 to 7% by weight of the sodium salt of the 5-beta-bromallyl-5'-isopropyl-N-methyl-barbituric acid, from 4 to 6% by weight of 1phenyl-2.B-dimethyl-pyrazolone, 5% by weight of glycerol, and from 2 to 5% by weight of diethyl-ether.

3. A liquid anesthetic agent for intravenous injection comprising an aqueuos solution of from 4 to 7% by weight of the sodium salt of the S-beta-bromallyl-S'-isopropyl-N-methyl-barbituric acid, from 4 to 6% by weight of 1-pheuyl-2.3-dimethyl-pyrazolone, 5% by weight of 1,2 propanediol, and from 2 to 5% by weight of diethylether.

4. A liquid anesthetic agent for intravenous injection comprising an aqueous solution of from 4 to 7% by weight or" the sodium salt of the S-beta-brornallyl-5-isopropyl-N-methyl barbituric acid, from 4 to 6% by weight of 1-phenyl-2.3-dimethyl-pyrazolone, 5% by weight of 1,3 butanediol, and from 2 to 5% by weight of diethyl-ether.

5. A liquid anesthetic agent for intravenous injection comprising an aqueous solution of from 4 to 7% by weight of the sodium salt of the 5-beta-bromallyl-5'-isopropyl-N-methyl-barbituric acid, from 4 to 6% by weight of l-phenyl-Z.S-dimethyl-pyrazolone, from 2 to 5% by weight of diethyl-ether, and from 4 to 6% by weight of a liquid selected from the group consisting of glycerol and of 1,2 propanediol and of 1,3 butanediol.

References Cited in the file of this patent UNITED STATES PATENTS Axelrod Sept. 26, 1933 Gruber Jan. 12, 1937 OTHER REFERENCES 

1. A LIQUID ANESTHETIC AGENT FOR INTRAVENOUS INJECTION COMPRISING AN AQUEOUS SOLUTION OF FROM 4 TO 7% BY WEIGHT OF THE SODIUM SALT OF THE 5-BETA-BROMALLYL-5''-ISOPROPYL-N-METHYL-BARBITURIC ACID, FROM 4 TO 6% BY WEIGHT OF 1-PHENYL-2.3-DIMETHYL-PYRAZOLONE, FROM 2 TO 5% BY WEIGHT OF DIETHYL-ETHER, AND 5% BY WEIGHT OF A LIQUID SELECTED FROM THE GROUP CONSISTING OF GLYCEROL AND OF 1,2 PROPANEDIOL AND OF 1,3 BUTANEDIOL. 